受注:045-509-1970 |
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Synonyms | Broussonpapyrine chloride | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C21H18NO4.HCl |
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分子量 | 384.83 | CAS No. | 3895-92-9 | |
Solubility (25°C)* | 体外 | DMSO | 3 mg/mL (7.79 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Chelerythrine Chloride (NSC 646662, Broussonpapyrine) is a potent, selective antagonist of PKC with IC50 of 0.66 mM. |
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in vitro | Chelerythrine interacts with the catalytic domain of PKC, is a competitive inhibitor with respect to the phosphate acceptor (histone IIIS) with Ki value of 0.7 μM and a non-competitive inhibitor with respect to ATP. Chelerythrine shows potent cytotoxic effects against L-1210 cells with IC50 of 0.53 μM. Chelerythrine does not alter any activity of PKA, TPK and Ca/CM-PK, and the Chelerythrine inhibitory effect on PKC activity does not vary among the various substrates including GS, MLC, MBP and Fibrinogen. [1] Chelerythrine inhibits PKC activity in crude cell extracts from SQ-20B cells in a dose dependent manner. Chelerythrine decreases cell viability as determined by the MTT assay in a dose-dependent manner in SCC35, JSQ3, SQ20B and SCC61 cells. [2] Chelerythrine chloride (5 μM) suppresses VEGF-induced expression of ICAM-1, VCAM-1, and E-selectin in HUVECs. Chelerythrine chloride (5 μM) suppresses VEGF-induced NF-κB activity in HUVECs. Chelerythrine chloride (5 μM) all suppresses basal and VEGF-induced leukocyte adhesiveness in HUVECs. [3] Chelerythrine (6 mM-30 mM) rapidly induces pyknosis, shrinkage and subsequent cell death in cardiac myocytes. Chelerythrine(30 μM)-induced myocyte death is accompanied by nuclear fragmentation and activation of caspase-3 and -9 in primary culture of neonatal rat ventricular myocytes. Chelerythrine (10 μM) causes cytochrome c release from mitochondria, suggesting that ROS mediates chelerythrine-induced cytochrome c release in cardiac myocytes. [4] Chelerythrine displaces the fluorescently labeled BH3 domain peptide from a recombinant GST-BcLXL fusion protein with IC50 of 1.5 μM. Chelerythrine at 2.5 μM and 5 μM for 16 hours induces a substantial decrease in mitochondrial potential as indicated by an increase in JC-1 green fluorescence in human neuroblastoma SH-SY5Y cells. Chelerythrine (5 μM) also induces the appearance of sub-G1 DNA that is indicative of apoptosis in SH-SY5Y cells. Chelerythrine (10 μM) induces mitochondrial potential change, CytC release from the mitochondria in SH-SY5Y cells. [5] |
in vivo | Chelerythrine (5 mg/kg i.p.) results in tumor growth delay in mice bearing SQ-20B xenografts. [2] Chelerythrine (5 mg/kg) treatment significantly increases TUNEL-positive nuclei in the myocardium as well as cleaved forms of caspase-3 and -9 in adult rat. [4] |
特徴 | Chelerythrine is at least 100-fold more selective for PKCs than for other kinases. |
キナーゼアッセイ | assay for protein kinase C | |
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The purified protein kinase C is prepared from rat brain. Briefly, the incubation mixture (200 μL) contains 20 mM Tris/HCl buffer (pH 7.5), 10 mM MgCl2, 200 μg/mL histones, micelles makes with 700 μM phosphatidyl serine and 180 μM 1,2-dioleine in 0.3% triton X100, 0.2 mM CaCl2, 100 μM ATP, [γ-32P ]-ATP (105 dpm), Chelerythrine to be tested (solubilized in dimethylsulphoxyde) and the enzyme (0.5 μg protein). After incubation at 30℃ for 3 minutes, the reaction is terminated by the addition of 3 mL of 20% trichloroacetic acid. Acid-precipitable materials are collected on Whatman GFE filters and extensively washed with ice-cold 20% trichloroacetic acid. The radioactivity on the filters is measured using a liquid scintillation counter. Protein kinase C activity is corrected for non-specific activity by assaying in the absence of micelles and CaCl2. | ||
細胞アッセイ | 細胞株 | L-1210 cells |
濃度 | ~10 μM | |
反応時間 | 2 days | |
実験の流れ | The lymphocytic mouse leukemia L1210 cells are plated sparsely at 1×104 cells per well in 24-well cluster plates in RPMI 1640 medium containing 10% foetal calf serum, 4 mM glutamine, 100 U/mL penicillin, 100 pg/mL streptomycin sulphate and Chelerythrine to be tested (solubilized in dimethylsulphoxyde ). After a 2 day incubation period at 37 ℃ in a humidified atmosphere (5% CO2 in air), growth is monitored by counting cell numbers in a coulter-counter. IC50 values are calculated on the basis of the linear regression lines established for Chelerythrine tested. |
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動物実験 | 動物モデル | mice bearing SQ-20B xenografts |
投薬量 | 5 mg/kg | |
投与方法 | Intraperitoneal injection |
Trace amine-associated receptor 1 regulation of Kv1.4 channels in trigeminal ganglion neurons contributes to nociceptive behaviors [ J Headache Pain, 2023, 24(1):49] | PubMed: 37158881 |
Effect of feeding regimen on circadian activity rhythms of food anticipatory by ghrelin hormone in a pig model [ Nutr Neurosci, 2022, 1-19] | PubMed: 35249475 |
An Early and Robust Activation of Caspases Heads Cells for a Regulated Form of Necrotic-like Cell Death [ J Biol Chem, 2015, 290(34):20841-55] | PubMed: 26124276 |
Signaling pathways of a structural analogue of apelin-12 involved in myocardial protection against ischemia/reperfusion injury [ Peptides, 2015, 73:67-76] | PubMed: 26348269 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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